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EP3778586A4 - Composé quinazoline servant d'inhibiteur de triple mutation d'egfr et ses applications - Google Patents

Composé quinazoline servant d'inhibiteur de triple mutation d'egfr et ses applications Download PDF

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Publication number
EP3778586A4
EP3778586A4 EP19785966.3A EP19785966A EP3778586A4 EP 3778586 A4 EP3778586 A4 EP 3778586A4 EP 19785966 A EP19785966 A EP 19785966A EP 3778586 A4 EP3778586 A4 EP 3778586A4
Authority
EP
European Patent Office
Prior art keywords
applications
compound serving
quinazoline compound
triple mutation
mutation inhibitor
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP19785966.3A
Other languages
German (de)
English (en)
Other versions
EP3778586A1 (fr
Inventor
Honglin Li
Jian Ding
Yufang Xu
Hua Xie
Qiannan LI
Tao Zhang
Zhenjiang ZHAO
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
East China University of Science and Technology
Original Assignee
East China University of Science and Technology
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by East China University of Science and Technology filed Critical East China University of Science and Technology
Publication of EP3778586A1 publication Critical patent/EP3778586A1/fr
Publication of EP3778586A4 publication Critical patent/EP3778586A4/fr
Withdrawn legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
EP19785966.3A 2018-04-13 2019-04-12 Composé quinazoline servant d'inhibiteur de triple mutation d'egfr et ses applications Withdrawn EP3778586A4 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201810332709.XA CN110372666B (zh) 2018-04-13 2018-04-13 喹唑啉类化合物作为egfr三突变抑制剂及其应用
PCT/CN2019/082498 WO2019196938A1 (fr) 2018-04-13 2019-04-12 Composé quinazoline servant d'inhibiteur de triple mutation d'egfr et ses applications

Publications (2)

Publication Number Publication Date
EP3778586A1 EP3778586A1 (fr) 2021-02-17
EP3778586A4 true EP3778586A4 (fr) 2022-03-16

Family

ID=68163006

Family Applications (1)

Application Number Title Priority Date Filing Date
EP19785966.3A Withdrawn EP3778586A4 (fr) 2018-04-13 2019-04-12 Composé quinazoline servant d'inhibiteur de triple mutation d'egfr et ses applications

Country Status (6)

Country Link
US (1) US20210155604A1 (fr)
EP (1) EP3778586A4 (fr)
JP (1) JP2021521215A (fr)
KR (1) KR20210003807A (fr)
CN (2) CN110372666B (fr)
WO (1) WO2019196938A1 (fr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112778217B (zh) * 2019-11-08 2024-01-26 沈阳化工研究院有限公司 一种喹唑啉类化合物及其应用
KR102267662B1 (ko) * 2019-11-19 2021-06-22 한국화학연구원 벤즈아미드 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
CN117126142A (zh) * 2023-08-30 2023-11-28 遵义医科大学珠海校区 杂环类egfr突变抑制剂及其应用
CN117800925A (zh) * 2023-10-25 2024-04-02 浙江工业大学 苯基脲基喹唑啉类化合物及制备和在制备预防或治疗肝癌药物中的应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004013091A2 (fr) * 2002-08-01 2004-02-12 Yissum Research Development Company Of The Hebrew University Of Jerusalem Quinazolines 4-anilido substituees et utilisation de celles-ci comme inhibiteurs des kinases du recepteur du facteur de croissance de l'epiderme
WO2006116713A1 (fr) * 2005-04-27 2006-11-02 Amgen Inc. Derives d'amides substitues en tant qu'inhibiteurs de la proteine kinase
WO2017004383A1 (fr) * 2015-06-30 2017-01-05 Dana-Farber Cancer Institute, Inc. Inhibiteurs d'egfr et méthodes d'utilisation de ceux-ci

Family Cites Families (12)

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Publication number Priority date Publication date Assignee Title
JPS5538325A (en) * 1978-09-11 1980-03-17 Sankyo Co Ltd 4-anilinoquinazoline derivative and its preparation
JP2002526538A (ja) * 1998-10-01 2002-08-20 アストラゼネカ アクチボラグ 化学化合物
US20030149045A1 (en) * 1999-08-20 2003-08-07 Fatih M Uckun Therapeutic compounds
AU7301000A (en) * 1999-09-21 2001-04-24 Astrazeneca Ab Quinazoline derivatives and their use as pharmaceuticals
TW200505452A (en) * 2003-06-17 2005-02-16 Astrazeneca Ab Chemical compounds
WO2010068951A1 (fr) * 2008-12-12 2010-06-17 Fox Chase Cancer Center Thérapie combinée basée sur l’inhibition de kinase src et aurora pour le traitement du cancer
CN102146059A (zh) * 2010-02-08 2011-08-10 上海艾力斯医药科技有限公司 喹唑啉衍生物、制备方法及其应用
CN103965120B (zh) * 2013-01-25 2016-08-17 上海医药集团股份有限公司 喹啉及喹唑啉衍生物、制备方法、中间体、组合物及应用
CN104230826B (zh) * 2013-06-08 2017-03-29 复旦大学 2‑氟代喹唑啉环类化合物及其制备方法和药用用途
CN104530063B (zh) * 2015-01-13 2017-01-18 北京赛特明强医药科技有限公司 喹唑啉并杂环类化合物及其制备方法和作为用于治疗癌症的表皮生长因子受体抑制剂的应用
CN107129506B (zh) * 2016-02-26 2019-10-22 华东理工大学 作为EGFR抑制剂的嘧啶并[4,5-d][1,3]噁嗪-2-酮衍生物及其应用
CN105884699B (zh) * 2016-05-11 2019-05-07 中国药科大学 4-取代苯胺喹唑啉类衍生物及其制备方法和用途

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004013091A2 (fr) * 2002-08-01 2004-02-12 Yissum Research Development Company Of The Hebrew University Of Jerusalem Quinazolines 4-anilido substituees et utilisation de celles-ci comme inhibiteurs des kinases du recepteur du facteur de croissance de l'epiderme
WO2006116713A1 (fr) * 2005-04-27 2006-11-02 Amgen Inc. Derives d'amides substitues en tant qu'inhibiteurs de la proteine kinase
WO2017004383A1 (fr) * 2015-06-30 2017-01-05 Dana-Farber Cancer Institute, Inc. Inhibiteurs d'egfr et méthodes d'utilisation de ceux-ci

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
LIU YU-JING ET AL: "Recent Developments of Small Molecule EGFR Inhibitors Based on the Quinazoline Core Scaffolds", ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, vol. 12, no. 4, 1 April 2012 (2012-04-01), NL, pages 391 - 406, XP055828705, ISSN: 1871-5206, DOI: 10.2174/187152012800228652 *
See also references of WO2019196938A1 *
ZHANG HAI-QI ET AL: "Design and discovery of 4-anilinoquinazoline-acylamino derivatives as EGFR and VEGFR-2 dual TK inhibitors", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, ELSEVIER, AMSTERDAM, NL, vol. 109, 20 December 2015 (2015-12-20), pages 371 - 379, XP029399588, ISSN: 0223-5234, DOI: 10.1016/J.EJMECH.2015.12.032 *

Also Published As

Publication number Publication date
CN110372666A (zh) 2019-10-25
US20210155604A1 (en) 2021-05-27
WO2019196938A1 (fr) 2019-10-17
CN112236422B (zh) 2023-05-16
CN112236422A (zh) 2021-01-15
KR20210003807A (ko) 2021-01-12
CN110372666B (zh) 2022-11-08
JP2021521215A (ja) 2021-08-26
EP3778586A1 (fr) 2021-02-17

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